Chemical Profile and Screening of Bioactive Metabolites of Rindera graeca (A. DC.) Bois. & Heldr. (Boraginaceae) In Vitro Cultures

Rindera graeca is a rare endemic plant where in vitro culture has been used in order to investigate bioactive metabolites. Phytochemical study of the in vitro shoots and hairy roots led to the isolation of seven phenolic derivatives and the unusual furano-naphthoquinone rinderol. R. graeca was also analyzed for its pyrrolizidine alkaloids content by LC-MS, and it was found to contain echinatine together with echinatine and rinderine N-oxides. Rinderol, isolated only from in vitro hairy root culture for the first time in the genus, revealed promising bioactivities. It was evaluated in vitro against a panel of microorganisms, showing very strong activity specifically against Gram-positive bacteria (MIC values 0.98 × 10−2–1.18 µg/mL) as well as very interesting antiproliferative effect against the human non-small-cell bronchopulmonary carcinoma cell line NSCLC-N6-L16 and the epidermoid lung cancer cell line A549. These findings were compared with the chemical profile of the plant from nature, while this study is the first to report on the effects of R. graeca extracts obtained from in vitro culture, providing a valuable contribution to the scientific community towards this sustainable method of production of potential bioactive molecules.

Download Full-text

Co-Crystals of Resveratrol and Polydatin with L-Proline: Crystal Structures, Dissolution Properties, and In Vitro Cytotoxicities

Molecules ◽

10.3390/molecules26185722 ◽

2021 ◽

Vol 26 (18) ◽

pp. 5722

Author(s):

Yijie Lou ◽

Kaxi Yu ◽

Xiajun Wu ◽

Zhaojun Wang ◽

Yusheng Cui ◽

...

Keyword(s):

Cell Line ◽

Chemical Properties ◽

Cancer Cell Line ◽

Lung Cancer Cell Line ◽

Hek 293 ◽

Dissolution Properties ◽

Diphenyltetrazolium Bromide ◽

Water Ph ◽

Physical And Chemical

Resveratrol (RSV) and polydatin (PD) have been widely used to treat several chronic diseases, such as atherosclerosis, pulmonary fibrosis, and diabetes, among several others. However, their low solubility hinders their further applications. In this work, we show that the solubility of PD can be boosted via its co-crystallization with L-proline (L-Pro). Two different phases of co-crystals, namely the RSV-L-Pro (RSV:L-Pro = 1:2) and PD-L-Pro (PD:L-Pro = 1: 3), have been prepared and characterized. As compared to the pristine RSV and PD, the solubility and dissolution rates of PD-L-Pro in water (pH 7.0) exhibited a 15.8% increase, whereas those of RSV-L-Pro exhibited a 13.8% decrease. A 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay of pristine RSV, PD, RSV-L-Pro, and PD-L-Pro against lung cancer cell line A549 and human embryonic kidney cell line HEK-293 indicated that both compounds showed obvious cytotoxicity against A549, but significantly reduced cytotoxicity against HEK-293, with PD/PD-L-Pro further exhibiting better biological safety than that of RSV/RSV-L-Pro. This work demonstrated that the readily available and biocompatible L-Pro can be a promising adjuvant to optimize the physical and chemical properties of RSV and PD to improve their pharmacokinetics.

Download Full-text

Curcumin composite particles prepared by spray drying and in vitro anti-cancer activity on lung cancer cell line

Journal of Drug Delivery Science and Technology ◽

10.1016/j.jddst.2018.04.006 ◽

2018 ◽

Vol 45 ◽

pp. 397-407 ◽

Cited By ~ 4

Author(s):

Thanu Thongnopkoon ◽

Chuda Chittasupho

Keyword(s):

Lung Cancer ◽

Cell Line ◽

Spray Drying ◽

Cancer Cell Line ◽

Lung Cancer Cell Line ◽

Composite Particles ◽

Lung Cancer Cell ◽

Anti Cancer ◽

Cancer Activity

Download Full-text

In vitro antitumor effect of cucurbitacin E on human lung cancer cell line and its molecular mechanism

Chinese Journal of Natural Medicines ◽

10.1016/s1875-5364(20)30058-3 ◽

2020 ◽

Vol 18 (7) ◽

pp. 483-490

Author(s):

Si-Yuan JING ◽

Zi-Dan WU ◽

Tie-Hua ZHANG ◽

Jie ZHANG ◽

Zheng-Yi WEI

Keyword(s):

Lung Cancer ◽

Cell Line ◽

Antitumor Effect ◽

Human Lung ◽

Cancer Cell Line ◽

Lung Cancer Cell Line ◽

Human Lung Cancer ◽

Lung Cancer Cell ◽

Cucurbitacin E

Download Full-text

Jaceidin Flavonoid Isolated from Chiliadenus montanus Attenuates Tumor Progression in Mice via VEGF Inhibition: In Vivo and In Silico Studies

Plants ◽

10.3390/plants9081031 ◽

2020 ◽

Vol 9 (8) ◽

pp. 1031 ◽

Cited By ~ 1

Author(s):

Sameh S. Elhady ◽

Enas E. Eltamany ◽

Amera E. Shaaban ◽

Alaa A. Bagalagel ◽

Yosra A. Muhammad ◽

...

Keyword(s):

Cell Line ◽

Cancer Cell ◽

In Silico ◽

Cancer Cell Line ◽

Control Group ◽

Phytochemical Study ◽

Aerial Parts ◽

In Silico Studies

Phytochemical study of Chiliadenus montanus aerial parts afforded six compounds; Intermedeol (1), 5α-hydroperoxy-β-eudesmol (2), 5,7-dihydroxy-3,3’,4’-trimethoxyflavone (3), 5,7,4’-trihydroxy-3,6,3’-trimethoxyflavone (jaceidin) (4), eudesm-11,13-ene-1β,4β,7α-triol (5) and 1β,4β,7β,11-tetrahydroxyeudesmane (6). These compounds were identified based on their NMR spectral data. The isolated compounds were tested for their cytotoxicity against liver cancer cell line (HepG2) and breast cancer cell line (MCF-7). Jaceidin flavonoid (4) exhibited the highest cytotoxic effect in vitro. Therefore, both of jaceidin and C. montanus extract were evaluated for their in vivo anti-tumor activity against Ehrlich’s ascites carcinoma (EAC). Compared to control group, jaceidin and C. montanus extract decreased the tumor weight, improved the histological picture of tumor cells, lowered the levels of VEGF and ameliorate the oxidative stress. Molecular docking and in silico studies suggested that jaceidin was a selective inhibitor of VEGF-mediated angiogenesis with excellent membrane permeability and oral bioavailability.

Download Full-text